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Folate preparations

A technology of compounds and preparations, applied in reducing folic acid compounds and in the field of eye disease management, can solve problems such as folic acid levels below normal levels, folic acid malabsorption, folic acid deficiency, etc.

Pending Publication Date: 2021-04-16
阿普罗福尔公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, intake of antimetabolites such as methotrexate, acetrexate, and alcohol abuse in cancer therapy, which are used as competitive inhibitors of dihydrofolate reductase, due to dietary folate malabsorption due to celiac disease, may cause folic acid deficiency
In addition, genetically established dysfunction of one or more folate-metabolizing enzymes may result in lower-than-normal folate levels

Method used

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  • Folate preparations
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Intraocular pressure was checked during two visits to an ophthalmologist in a female patient with pseudoexfoliation glaucoma (PEX). The first checkup was done on March 05, 2019, and IOP was found to be 15mm Hg (right eye) and 15mm Hg (left eye). From May 1, 2019 to August 21, 2019, the patient took one tablet forte capsules, the composition of which is shown below. During the second intraocular pressure check on August 13, 2019, the intraocular pressure measurement gave the following results, 12mm Hg (right eye) and 12mm Hg (left eye).

[0066] in daily intake The reduction in IOP from 15mm Hg to 12mm Hg during about 3 months of the forte is a significant reduction, even considering that an IOP of 15mm Hg is in the range of 12mm Hg to 20mm Hg, which is considered normal. forte is a formulation comprising L-5-methyl-folic acid, respectively its calcium salt. The composition, respectively, the amount of its active ingredient is shown below.

[0067] Compounds form...

Embodiment 2

[0071] The table below presents the results of seven exemplary patients who participated in a study designed to evaluate the effect of 12 weeks (1 capsule per day) of a formulation containing L-methylfolate on the eyes in patients with diabetes. Effects on blood pressure, total ocular blood flow, and systemic homocysteine ​​plasma concentrations. The formulations used in this study containing at least one reduced form of folate were forte. The composition is as shown in Example 1. In addition to containing 25 mg of zinc in the form of zinc acetate.

[0072]The systolic, diastolic and mean blood pressure (SBP, DBP, MAP) of the upper arm were measured by an automatic oscillometric device. Pulse rate is recorded automatically by a finger pulse oximeter.

[0073] Intraocular pressure was measured with a Goldmann applanation tonometer equipped with a slit lamp. One drop of oxybuprocain hydrochloride combined with sodium fluorescein was used for local anesthesia of the cornea ...

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Abstract

The present invention relates to preparations of folate for use in the treatment of eye disorders in the presence of elevated intraocular pressure.

Description

technical field [0001] The present invention relates to reduced folates and their use in the management of eye diseases. Background technique [0002] Diseases and degenerative conditions of the optic nerve and retina are the leading causes of blindness in the world. Worldwide, approximately 300 million people suffer from various forms of vision impairment caused by these diseases. The most common disorders are optic neuropathy, retinopathy, and glaucoma. [0003] There are many forms of optic neuropathy. One form is toxic neuropathy, in which damage to the optic nerve is caused by toxic compounds such as methanol. Another form is nutritional neuropathy caused by nutritional deficiencies of one or more micronutrients such as folate and other B vitamins. Current approaches to managing nutritional deficiencies are often based on oral supplements. However, in the case of the eye, this approach may not always be effective because the blood-retinal barrier (BRB) in the retin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61K31/047A61K31/065A61K31/197A61K31/198A61K31/355A61K31/375A61K31/51A61K31/525A61K31/593A61K31/675A61K31/714A61K33/04A61K33/30A61K33/34A61P27/06
CPCA61K31/047A61K31/065A61K31/197A61K31/198A61K31/355A61K31/375A61K31/51A61K31/519A61K31/525A61K31/593A61K31/675A61K31/714A61K33/04A61K33/30A61K33/34A61K36/752A61P27/06A61K2300/00A61K9/0048A61K9/08
Inventor 马丁·乌尔曼格尔德·威斯勒约瑟夫·弗拉默尔
Owner 阿普罗福尔公司
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